Motesanib | CAS 453562-69-1 (free base)

Motesanib

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
250mg	$950	Check With Us
500mg	$1650	Check With Us
1g	$2475	Check With Us

: [email protected] [email protected]

Cat #: V4082 CAS #: 453562-69-1 (free base) Purity ≥ 98%

Description: Motesanib (formerly also known as AMG-706) is a novel, potent, ATP-competitive, orally bioavailable inhibitor of VEGFR1/2/3 (vascular endothelial growth factor) with IC50 of 2 nM/3 nM/6 nM, respectively; it has potential anticancer activity; Motesanib shows similar activity against Kit, and ~10-fold more selective for VEGFR than PDGFR and Ret.

References: Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer R

Top Publications Citing Invivochem Products

Product Catalog 2022

Guide to Product Handling

Publications Citing InvivoChem Products

Product Promise

Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	373.46
Molecular Formula	C22H23N5O
CAS No.	453562-69-1 (free base)
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: >30 mg/mLr
	Water: N/Ar
	Ethanol: N/A
SMILES Code	O=C(C1=CC=CN=C1NCC2=CC=NC=C2)NC3=CC4=C(C=C3)C(C)(C)CN4
Synonyms	AMG-706; AMG 706; AMG706

Protocol	In Vitro	Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC50 of >3,000 nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells.
Protocol	In Vivo	Motesanib (100 mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.6777 mL	13.3883 mL	26.7766 mL	53.5533 mL
5mM	0.5355 mL	2.6777 mL	5.3553 mL	10.7107 mL
10mM	0.2678 mL	1.3388 mL	2.6777 mL	5.3553 mL
20mM	0.1339 mL	0.6694 mL	1.3388 mL	2.6777 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.